Biophysical Insights into the Inhibitory Mechanism of Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors

Biomolecules

Grant Schauer¹  Sanford Leuba¹ 

[1] Program in Molecular Biophysics and Structural Biology, Hillman Cancer Center, University of Pittsburgh, 5117 Centre Ave., Pittsburgh, PA 15213, USA; E-Mails:

关键词: HIV-1 reverse transcriptase;    NNRTI;    mechanism;    biophysics;    single-molecule;   

DOI  :  10.3390/biom3040889

来源: mdpi

【 摘 要 】

HIV-1 reverse transcriptase (RT) plays a central role in HIV infection. Current United States Federal Drug Administration (USFDA)-approved antiretroviral therapies can include one of five approved non-nucleoside RT inhibitors (NNRTIs), which are potent inhibitors of RT activity. Despite their crucial clinical role in treating and preventing HIV-1 infection, their mechanism of action remains elusive. In this review, we introduce RT and highlight major advances from experimental and computational biophysical experiments toward an understanding of RT function and the inhibitory mechanism(s) of NNRTIs.

【 授权许可】

CC BY   
© 2013 by the authors; licensee MDPI, Basel, Switzerland.